2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑

生物活性靶点体外研究体内研究 2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑试剂级价格

CAS号:40045-50-9
英文名:5-[(5-Nitro-2-thiazolyl)thio]-1,3,4thiadiazol-2-amine
中文名:2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑
CBNumber:CB42518901
分子式:C5H3N5O2S3
分子量:261.3
MOL File:40045-50-9.mol

2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑化学性质

熔点 :160 °C(dec.)
沸点 :549.8±42.0 °C(Predicted)
密度 :1.88±0.1 g/cm3(Predicted)
储存条件 :Store at RT
溶解度 :DMSO : 62.5 mg/mL (239.19 mM; Need ultrasonic)
形态 :Pale yellow solid
酸度系数(pKa) :0.65±0.10(Predicted)
颜色 :Light yellow to Amber to Dark green
InChI :InChI=1S/C5H3N5O2S3/c6-3-8-9-5(14-3)15-4-7-1-2(13-4)10(11)12/h1H,(H2,6,8)
InChIKey :NQQBNZBOOHHVQP-UHFFFAOYSA-N
SMILES :S1C(SC2=NC=C([N+]([O-])=O)S2)=NN=C1N

安全信息

海关编码 :2934100090

2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑性质、用途与生产工艺

生物活性 SU3327 是一种有效的，选择性的且具有底物竞争性的 JNK 抑制剂，IC50 为 0.7 μM。SU3327 还以 IC50 值为 239 nM 抑制 JNK 和 JIP 之间的蛋白相互作用。SU3327 对 p38α 和 Akt 激酶的活性较低。
靶点

IC50: 0.7 μM (JNK); 239 nM (JNK-JIP interactions)
体外研究

SU3327 (compound 9) is able to inhibit TNF-α stimulated phosphorylation of c-Jun in HeLa cells (EC ₅₀ = 6.23 μM).
SU3327 (25 nM) pretreatment of human-derived cerebral microvascular endothelial cells (hCMEC/D3) effectively reduces LPS-induced polymorphonuclear leukocytes (PMN) rolling/adhesion to hCMEC/D3, prevents activation of AP-1, and significantly reduces expression of VCAM-1.

体内研究

SU3327 (Compound 9; 25 mg/kg; intraperitoneal injection; male BKS.Cg-+Lepr ^db /+Lepr ^db /OlaHsd db/db mice) treatment possesses the ability to restore insulin sensitivity in mice models of diabetes.
SU3327 (Compound 9) has favorable microsomal and plasma stability (T _1/2 = 27 min).

Animal Model:	Male BKS.Cg-+Lepr ^db /+Lepr ^db /OlaHsd db/db mice (11-week-old ) injected with insulin
Dosage:	25 mg/kg
Administration:	Intraperitoneal injection
Result:	Resulted in a statistically significant reduction in blood glucose levels.